Spirocyclic scaffolds in medicinal chemistry

K Hiesinger, D Dar'in, E Proschak… - Journal of Medicinal …, 2020 - ACS Publications
Spirocyclic scaffolds are incorporated in various approved drugs and drug candidates. The
increasing interest in less planar bioactive compounds has given rise to the development of …

Pyrrolidine in drug discovery: a versatile scaffold for novel biologically active compounds

G Li Petri, MV Raimondi, V Spanò, R Holl… - Topics in Current …, 2021 - Springer
The five-membered pyrrolidine ring is one of the nitrogen heterocycles used widely by
medicinal chemists to obtain compounds for the treatment of human diseases. The great …

Novel spiroindoline derivatives targeting aldose reductase against diabetic complications: bioactivity, cytotoxicity, and molecular modeling studies

Ö Güleç, C Türkeş, M Arslan, Y Demir, B Dincer… - Bioorganic …, 2024 - Elsevier
Despite significant developments in therapeutic strategies, Diabetes Mellitus remains an
increasing concern, leading to various complications, eg, cataracts, neuropathy, retinopathy …

Structural characterization of the millennial antibacterial (fluoro) quinolones—sha** the fifth generation

A Rusu, IA Lungu, OL Moldovan, C Tanase, G Hancu - Pharmaceutics, 2021 - mdpi.com
The evolution of the class of antibacterial quinolones includes the introduction in therapy of
highly successful compounds. Although many representatives were withdrawn due to …

ipso-Cyclization of unactivated biaryl ynones leading to thio-functionalized spirocyclic enones

CR Reddy, U Ajaykumar, AD Patil… - Organic & Biomolecular …, 2023 - pubs.rsc.org
Ceric ammonium nitrate (CAN)-promoted oxidative ipso-cyclization of unactivated biaryl
ynones with S-centered radicals (SCN/SCF3) to access spiro [5, 5] trienones has been …

Spiro-Flavonoids in Nature: A Critical Review of Structural Diversity and Bioactivity

Ł Pecio, S Pecio, T Mroczek, W Oleszek - Molecules, 2023 - mdpi.com
Based on the literature data from 1973 to 2022, this work summarizes reports on spiro-
flavonoids with a spiro-carbon at the center of their structure and how this affects their …

Recent advances in catalytic enantioselective synthesis of pyrazolones with a tetrasubstituted stereogenic center at the 4-position

L Carceller-Ferrer, G Blay, JR Pedro, C Vila - Synthesis, 2021 - thieme-connect.com
Pyrazolone [2, 4-dihydro-3H-pyrazol-4-one] represents one of the most important five-
membered nitrogen heterocycles which is present in numerous pharmaceutical drugs and …

Novel spiroindoline HDAC inhibitors: Synthesis, molecular modelling and biological studies

M Brindisi, J Senger, C Cavella, A Grillo… - European Journal of …, 2018 - Elsevier
This paper describes the rational development of a series of novel spiroindoline derivatives
endowed with selective inhibitory activity on the HDAC6 isoform. A convenient …

Enantioselective Synthesis of Functionalized Diazaspirocycles from 4‐Benzylideneisoxazol‐5(4H)‐one Derivatives and Isocyanoacetate Esters

P Martínez‐Pardo, A Laviós… - Advanced Synthesis …, 2020 - Wiley Online Library
Enantioenriched spirocyclic compounds bearing three contiguous stereocenters and high
functionalization were obtained through a formal [3+ 2] cycloaddition reaction catalyzed by a …

Design, synthesis, and biological evaluation of novel spirocyclic compounds as potential anti-glioblastoma agents

H Zhu, X Song, Y Pan, M Li, L Chen, P **ao… - European Journal of …, 2023 - Elsevier
Glioblastoma (GBM) is an aggressive brain tumor with extremely limited clinical treatment
options. Because of the blood–brain barrier (BBB), it is difficult for anti-GBM drug candidates …